CGP-42112

Research use only, not for human use.

CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM.

CGP-42112 (CGP42112A) is a highly potent, selective Angiotensin-II subtype 2 receptor(AT2 receptor) agonist with Ki of 0.24 nM; significantly inhibits cGMP production from the basal value, also significantly inhibits TH-enzyme activity from the basal value in cultured porcine adrenal medullary cells; antagonizes Ang-II induced contractions in rabbit aortic rings with IC50 of 1.85 uM.

CGP-42112 (≥1 nM) significantly inhibits cGMP production from the basal value. CGP-42112 (≥1 nM) significantly inhibits TH-enzyme activity from the basal value. These inhibitory effects of CGP-42112 on TH-enzyme activity and-cGMP production are abolished by PD123319 (AT(2)-R antagonist) while CV-11974 (AT(1)-R antagonist) is ineffective. CGP-42112 binds selectively to the AT2 angiotensin II receptor subtype. [125I]CGP-42112 binds with higher affinity in the brain than in the adrenal. beta-Mercaptoethanol enhanced [125I]CGP-42112 binding in the brain, but does not alter its binding in the adrenal. CGP-42112 binds with high affinity (Kd = 0.07-0.3 nM, depending on the area studied). CGP-42112 binding is selective for AT2 receptors, as determined by lack of competition with the AT1 ligand losartan, and competition by the AT2 ligands PD 123177 and unlabeled CGP-42112 and the non-selective peptides Ang II and angiotensin III (Ang III).

Intravenous infusions of CGP-42112 (0.1 and 1 mg kg-1 min-1) and PD 123319 (0.36 and 1 mg kg-1 min-1) shifted the upper limit of CBF autoregulation toward higher blood pressures without affecting baseline CBF.

CGP42112 | CGP 42112 | CGP-42112A

GPCR/G Protein

Angiotensin Receptor

Angiotensin Receptor

Neurological Disease

——

127060-75-7

1052.185

C52H69N13O11

>98% (HPLC)

DMSO: ≥ 350 mg/mL

CC[C@H](C)[C@@H](C(O)=O)NC([C@H]1N(C([C@H](CC2=CNC=N2)NC([C@H](CCCCNC([C@H](CCCNC(N)=N)NC(OCC3=CC=CC=C3)=O)=O)NC([C@H](CC4=CC=C(O)C=C4)NC(C5=CC=CN=C5)=O)=O)=O)=O)CCC1)=O

L-Isoleucine, N-(3-pyridinylcarbonyl)-L-tyrosyl-N6-[N2-[(phenylmethoxy)carbonyl]-L-arginyl]-L-lysyl-L-histidyl-L-prolyl-

(-20℃)

With Ice Pack

≥ 2 years